WO2000040247A8 - 2-amino-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite - Google Patents

2-amino-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite

Info

Publication number
WO2000040247A8
WO2000040247A8 PCT/GB2000/000032 GB0000032W WO0040247A8 WO 2000040247 A8 WO2000040247 A8 WO 2000040247A8 GB 0000032 W GB0000032 W GB 0000032W WO 0040247 A8 WO0040247 A8 WO 0040247A8
Authority
WO
WIPO (PCT)
Prior art keywords
reduced
formula
obesity
treatment
inhibition
Prior art date
Application number
PCT/GB2000/000032
Other languages
English (en)
Other versions
WO2000040247A1 (fr
WO2000040247A9 (fr
Inventor
Harold Francis Hodson
Robert Downham
Timothy John Mitchell
Beverley Jane Carr
Christopher Robert Dunk
Richard Michael John Palmer
Original Assignee
Alizyme Therapeutics Ltd
Harold Francis Hodson
Robert Downham
Timothy John Mitchell
Beverley Jane Carr
Christopher Robert Dunk
Richard Michael John Palmer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9900413.7A external-priority patent/GB9900413D0/en
Priority claimed from GBGB9917294.2A external-priority patent/GB9917294D0/en
Priority to DK00900082T priority Critical patent/DK1143977T3/da
Priority to ES00900082T priority patent/ES2240052T7/es
Application filed by Alizyme Therapeutics Ltd, Harold Francis Hodson, Robert Downham, Timothy John Mitchell, Beverley Jane Carr, Christopher Robert Dunk, Richard Michael John Palmer filed Critical Alizyme Therapeutics Ltd
Priority to CA002359819A priority patent/CA2359819C/fr
Priority to EP00900082A priority patent/EP1143977B3/fr
Priority to CH00900082T priority patent/CH1143977H1/fr
Priority to AT00900082T priority patent/ATE293447T1/de
Priority to NZ512740A priority patent/NZ512740A/en
Priority to MXPA01006921A priority patent/MXPA01006921A/es
Priority to DE60019555T priority patent/DE60019555C5/de
Priority to JP2000592004A priority patent/JP3822439B2/ja
Priority to SI200030683T priority patent/SI1143977T1/xx
Priority to AU18846/00A priority patent/AU765147C/en
Publication of WO2000040247A1 publication Critical patent/WO2000040247A1/fr
Publication of WO2000040247A8 publication Critical patent/WO2000040247A8/fr
Priority to NO20013381A priority patent/NO333922B1/no
Priority to US09/901,887 priority patent/US6624161B2/en
Publication of WO2000040247A9 publication Critical patent/WO2000040247A9/fr
Priority to US10/306,377 priority patent/US7825113B2/en
Priority to HK02109053.3A priority patent/HK1047588B/zh
Priority to US12/044,318 priority patent/US7858617B2/en
Priority to US12/952,972 priority patent/US8877750B2/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/24—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
    • C07D265/26—Two oxygen atoms, e.g. isatoic anhydride
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne l'utilisation d'un composé de formule (I) ou d'un sel, d'un ester, d'un amide ou d'un promédicament dudit composé, pour inhiber une enzyme dont le mode d'action préféré est de catalyser l'hydrolyse d'une fonctionnalité ester, par exemple pour la régulation et l'inhibition des enzymes indésirables dans les produits et les processus. Ces composés sont également utiles en médecine, par exemple pour le traitement de l'obésité et des pathologies voisines. L'invention concerne également des composés de formule (I), des procédés permettant de les préparer et des compositions pharmaceutiques les contenant. Dans la formule (I) A est un noyau aromatique ou hétéro-aromatique à 6 éléments; et R1 est alkyle ramifié ou non ramifié (éventuellement interrompu par un ou plusieurs atomes d'oxygène), alcényle, alcinyle, cycloalkyle, cycloalcényle, aryle, arylalkyle, arylalkyle réduit, arylalcényle, hétéroaryle, hétéro-arylalkyle, hétéro-arylalcényle, aryle réduit, hétéro-aryle réduit, hétéro-arylalkyle réduit, ou un dérivé substitué de l'un des groupes ci-dessus.
PCT/GB2000/000032 1999-01-08 2000-01-06 2-amino-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite WO2000040247A1 (fr)

Priority Applications (18)

Application Number Priority Date Filing Date Title
JP2000592004A JP3822439B2 (ja) 1999-01-08 2000-01-06 肥満治療用２−オキシ−４ｈ−３，１−ベンゾオキサジン−４−オン
MXPA01006921A MXPA01006921A (es) 1999-01-08 2000-01-06 Derivados de 2-oxi-benzoxazinona para el tratamiento de la obesidad.
SI200030683T SI1143977T1 (fr) 1999-01-08 2000-01-06
ES00900082T ES2240052T7 (es) 1999-01-08 2000-01-06 Derivados de 2-oxi benzoxazinona para el tratamiento de la obesidad
CA002359819A CA2359819C (fr) 1999-01-08 2000-01-06 2-amino-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite
EP00900082A EP1143977B3 (fr) 1999-01-08 2000-01-06 2-oxy-benzoxazine-4-ones destinees au traitement de l'obesite
CH00900082T CH1143977H1 (fr) 1999-01-08 2000-01-06 2-Oxy-benzoxazine-4-ones destinees au traitement de l'obesite
AT00900082T ATE293447T1 (de) 1999-01-08 2000-01-06 2-oxy-benzoxazinonderivate zur behandlung von fettleibigkeit
NZ512740A NZ512740A (en) 1999-01-08 2000-01-06 2-oxy-benzoxazinone derivatives for the treatment of obesity
AU18846/00A AU765147C (en) 1999-01-08 2000-01-06 2-Oxy-4H-3,1-Benzoxazin-4-Ones for the treatment of obesity
DE60019555T DE60019555C5 (de) 1999-01-08 2000-01-06 2-oxy-benzoxazinonderivate zur behandlung von fettleibigkeit
DK00900082T DK1143977T3 (da) 1999-01-08 2000-01-06 2-oxy-benzoxazinonderivater til behandling af obesitas
US09/901,887 US6624161B2 (en) 1999-01-08 2001-07-06 2-Oxy-benzoxazinone derivatives for the treatment of obesity
NO20013381A NO333922B1 (no) 1999-01-08 2001-07-06 2-oksybenzoksazinonderivater, fremgangsmåte for fremstilling, anvendelse derav for fremstilling av et medikament for behandling av fedme samt farmasøytisk preparat og matprodukt omfattende forbindelsen
US10/306,377 US7825113B2 (en) 1999-01-08 2002-11-27 2-oxy-benzoxazinone derivatives for the treatment of obesity
HK02109053.3A HK1047588B (zh) 1999-01-08 2002-12-13 治療肥胖症的2-氧-4h-3，1-苯並噁嗪-4-酮
US12/044,318 US7858617B2 (en) 1999-01-08 2008-03-07 2-oxy-benzoxazinone derivatives for the treatment of obesity
US12/952,972 US8877750B2 (en) 1999-01-08 2010-11-23 2-oxy-benzoxazinone derivatives for the treatment of obesity

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB9900413.7A GB9900413D0 (en) 1999-01-08 1999-01-08 Inhibitors
GB9900413.7 1999-01-08
GB9917294.2 1999-07-22
GBGB9917294.2A GB9917294D0 (en) 1999-07-22 1999-07-22 Inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US09/901,887 Continuation US6624161B2 (en) 1999-01-08 2001-07-06 2-Oxy-benzoxazinone derivatives for the treatment of obesity

Publications (3)

Publication Number Publication Date
WO2000040247A1 WO2000040247A1 (fr) 2000-07-13
WO2000040247A8 true WO2000040247A8 (fr) 2001-02-15
WO2000040247A9 WO2000040247A9 (fr) 2002-10-24

Family

ID=26314965

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2000/000032 WO2000040247A1 (fr) 1999-01-08 2000-01-06 2-amino-4h-3,1-benzoxazine-4-ones destinees au traitement de l'obesite

Country Status (24)

Country Link
US (4) US6624161B2 (fr)
EP (1) EP1143977B3 (fr)
JP (1) JP3822439B2 (fr)
KR (1) KR100678998B1 (fr)
CN (2) CN1315813C (fr)
AR (1) AR022204A1 (fr)
AT (1) ATE293447T1 (fr)
AU (1) AU765147C (fr)
CA (1) CA2359819C (fr)
CH (1) CH1143977H1 (fr)
DE (1) DE60019555C5 (fr)
DK (1) DK1143977T3 (fr)
ES (1) ES2240052T7 (fr)
HK (2) HK1047588B (fr)
HU (1) HUP0105003A3 (fr)
MX (1) MXPA01006921A (fr)
MY (1) MY122578A (fr)
NO (1) NO333922B1 (fr)
NZ (1) NZ512740A (fr)
PL (1) PL207383B1 (fr)
PT (1) PT1143977E (fr)
RU (1) RU2245331C2 (fr)
SI (1) SI1143977T1 (fr)
WO (1) WO2000040247A1 (fr)

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AR022204A1 (es) * 1999-01-08 2002-09-04 Norgine Bv Compuesto, proceso para su preparacion, composicion farmaceutica y producto comestible que lo comprende.
GB0001572D0 (en) 2000-01-24 2000-03-15 Alizyme Therapeutics Ltd Inhibitors
US6504028B2 (en) * 2000-07-11 2003-01-07 The Procter & Gamble Co. Process for preparing benzoxazin-4-one polymer conjugates
EP1425029A4 (fr) 2001-08-10 2006-06-07 Palatin Technologies Inc Peptidomimetiques de metallopeptides biologiquement actifs
MXPA04001922A (es) * 2001-08-30 2005-03-07 Alizyme Therapeutics Ltd Tieno-(1,3)-oxazin-4-onas con actividad inhibidora de lipasa.
AU2002366810B2 (en) * 2001-12-20 2009-06-11 Osi Pharmaceuticals, Inc. Pancreatic lipase inhibitor compounds, their synthesis and use
US8372430B2 (en) 2002-12-17 2013-02-12 The Procter & Gamble Company Compositions, methods, and kits useful for the alleviation of gastrointestinal effects
AU2004246895A1 (en) * 2003-06-12 2004-12-23 Biomas Ltd. Methods of treating obesity and related disorders using tellurium and selenium compounds
GB0319124D0 (en) * 2003-08-14 2003-09-17 Smithkline Beecham Corp Chemical compounds
US20050239859A2 (en) * 2003-09-03 2005-10-27 Solvay Pharmaceuticals Gmbh Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity
US20050124660A1 (en) * 2003-10-27 2005-06-09 Jochen Antel Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds
US20050143441A1 (en) * 2003-10-27 2005-06-30 Jochen Antel Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
US20050244367A1 (en) * 2004-05-03 2005-11-03 Ilypsa, Inc. Phospholipase inhibitors localized in the gastrointestinal lumen
WO2006045799A2 (fr) 2004-10-25 2006-05-04 Solvay Pharmaceuticals Gmbh Compositions pharmaceutiques contenant des antagonistes des recepteurs cannabinoides et des agents d'ouverture de canaux potassiques dans le traitement du diabete insulino-dependant, de l'obesite et des etats associes
WO2006116773A2 (fr) * 2005-04-28 2006-11-02 The Regents Of The University Of California Procedes, compositions et composes de modulation de la lipase de monoacylglycerol, de douleurs et de troubles lies au stress
US20090208584A1 (en) * 2005-06-09 2009-08-20 Tomohiro Yoshinari Solid preparation
JP2010254623A (ja) 2009-04-24 2010-11-11 Takeda Chem Ind Ltd ベンゾオキサジノン化合物の結晶
ES2662710T3 (es) 2010-05-24 2018-04-09 Swedish Oat Fiber Ab Dispersión acuosa que comprende galactolípidos y método de producción de la misma
AU2012101841A4 (en) * 2011-12-23 2013-01-17 Norgine Bv Compositions comprising cetilistat
WO2013092786A1 (fr) 2011-12-23 2013-06-27 Norgine B.V. Compositions comprenant du cetilistat
DE202012104963U1 (de) 2012-12-19 2013-01-14 Norgine B.V. Cetilistat aufweisende Zusammensetzungen
CN103936687B (zh) * 2014-03-24 2016-03-30 重庆东得医药科技有限公司 一种制备西替利司他的方法
CN104374836A (zh) * 2014-09-19 2015-02-25 安徽安科生物工程（集团）股份有限公司 西替利司他及有关杂质的hplc测定方法
CN105622538B (zh) * 2014-10-27 2019-02-01 中国医学科学院药物研究所 一锅法高收率制备新利司他
CN104341370B (zh) * 2014-11-11 2017-02-22 山东创新药物研发有限公司 一种西替利司他的制备方法
CN105566164A (zh) * 2016-01-06 2016-05-11 北京修正创新药物研究院有限公司 一种新利司他杂质的制备方法
CN105669585A (zh) * 2016-01-06 2016-06-15 北京修正创新药物研究院有限公司 一种新利司他的制备方法
WO2018011676A1 (fr) * 2016-07-11 2018-01-18 Symed Labs Limited Nouveaux procédés de préparation de dérivés de 2-oxy-benzoxazinone

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Also Published As

Publication number Publication date
US20080161301A1 (en) 2008-07-03
AU765147C (en) 2007-05-31
NO20013381L (no) 2001-09-07
CA2359819C (fr) 2008-08-12
HK1047588A1 (en) 2003-04-24
US6624161B2 (en) 2003-09-23
PL207383B1 (pl) 2010-12-31
CA2359819A1 (fr) 2000-07-13
NO333922B1 (no) 2013-10-21
KR100678998B1 (ko) 2007-02-07
US20110065697A1 (en) 2011-03-17
US20030195206A1 (en) 2003-10-16
MY122578A (en) 2006-04-29
JP3822439B2 (ja) 2006-09-20
US7825113B2 (en) 2010-11-02
US8877750B2 (en) 2014-11-04
NO20013381D0 (no) 2001-07-06
WO2000040247A1 (fr) 2000-07-13
JP2002534388A (ja) 2002-10-15
CH1143977H1 (fr) 2007-02-15
EP1143977B3 (fr) 2012-10-24
CN1315813C (zh) 2007-05-16
SI1143977T1 (fr) 2005-08-31
MXPA01006921A (es) 2003-06-04
HK1047588B (zh) 2007-08-24
ES2240052T3 (es) 2005-10-16
HUP0105003A2 (en) 2002-06-29
US7858617B2 (en) 2010-12-28
PT1143977E (pt) 2005-08-31
DE60019555T2 (de) 2006-02-23
ES2240052T7 (es) 2013-02-14
US20030027821A1 (en) 2003-02-06
CN1915981A (zh) 2007-02-21
CN1915981B (zh) 2011-09-28
HK1103928A1 (en) 2007-12-28
EP1143977A1 (fr) 2001-10-17
HUP0105003A3 (en) 2004-11-29
AU765147B2 (en) 2003-09-11
EP1143977B1 (fr) 2005-04-20
NZ512740A (en) 2003-10-31
AR022204A1 (es) 2002-09-04
CN1359378A (zh) 2002-07-17
ATE293447T1 (de) 2005-05-15
DE60019555D1 (de) 2005-05-25
DK1143977T3 (da) 2005-08-15
KR20020000542A (ko) 2002-01-05
RU2245331C2 (ru) 2005-01-27
DE60019555C5 (de) 2009-07-09
WO2000040247A9 (fr) 2002-10-24
AU1884600A (en) 2000-07-24

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